Effects of bifemelane on muscarinic receptors and choline acetyltransferase in the brains of aged rats following chronic cerebral hypoperfusion induced by permanent occlusion of bilateral carotid arteries.
Effects of bifemelane on muscarinic receptors and choline acetyltransferase in the brains of aged rats following chronic cerebral hypoperfusion induced by permanent occlusion of bilateral carotid arteries.
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比芬美烷对双侧颈动脉永久闭塞引起的慢性脑灌注不足的老年大鼠脑中毒蕈碱受体和胆碱乙酰转移酶的影响。
DOI：
10.1254/jjp.72.57
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发表时间：
1996
期刊：
影响因子：
--
通讯作者：
Y. Yamanaka
中科院分区：
文献类型：
--
作者：
T. Egashira;F. Takayama;Y. Yamanaka
通过永久双侧颈总动脉（2VO）永久闭塞老年大鼠，长期诱发脑灌注不足。与对照组老年大鼠相比，皮层和纹状体中毒蕈碱受体（mAChR）的Bmax值以及皮质、海马和纹状体中胆碱乙酰转移酶（ChAT）活性的Vmax值显着降低。在年轻对照大鼠和年轻 2VO 大鼠之间未观察到 mAChR 和 ChAT 活性的显着变化。老年大鼠术后 1 个月，在 4 周内每日口服比芬美兰 (10 mg/kg) 或阿尼拉西坦 (50 mg/kg)。施用联苯美烷显着增加纹状体 mAChR 中 3H-奎宁环苯甲酸 (QNB) 的 Bmax 值并降低表观 Kd 值。长期服用比芬美兰或阿尼西坦也增强了皮质、海马和纹状体的 ChAT 活性。特别是，给予 bifemelane 导致所有三个脑区 ChAT 的 Vmax 值显着增加，而 ChAT 的 K(m) 值没有观察到显着变化。这些结果表明，bifemelane 负责这种活性，从而增强脑灌注不足的老年大鼠的中枢神经系统胆碱能神经元的功能系统。
Cerebral hypoperfusion was chronically induced in aged rats via permanent bilateral occlusion of common carotid arteries (2VO). Marked reduction of the Bmax value of the muscarinic receptors (mAChR) in both the cortex and striatum and the Vmax value of choline acetyltransferase (ChAT) activity in the cortex, hippocampus and striatum were observed as compared with those of control aged rats. No significant changes in mAChR and ChAT activity were observed between young control rats and young 2VO rats. One month post-surgery in aged rats, daily doses of bifemelane (10 mg/kg) or aniracetam (50 mg/kg) were administered orally over a 4-week period. Administration of bifemelane significantly increased Bmax values and decreased apparent Kd values for 3H-quinuclidinyl benzilate (QNB) in mAChR in the striatum. Chronic administration of bifemelane or aniracetam also enhanced ChAT activity in the cortex, hippocampus and striatum. In particular, administration of bifemelane resulted in a significant increase in Vmax values of ChAT in all three brain regions, while no significant change in K(m) values for ChAT was observed. These results suggest that bifemelane is responsible for this activity, thereby enhancing the functioning system of CNS cholinergic neurons of cerebral hypoperfused aged rats.